Ricardo A. M. Serafim*, and , Matthias Gehringer*,
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引用次数: 0
Abstract
Protein kinases are highly relevant drug targets, yet a significant fraction of the human kinome remains underexplored. Highly potent and selective small-molecule inhibitors used as chemical probes are invaluable tools for enabling the validation and translation of new kinase targets. This review provides an overview and analysis of the high-quality in vivo chemical probes for protein kinases published and deposited at the Chemical Probes Portal in the year 2024. We discuss the design strategies, molecular mechanism of action, details of their use in vitro and in vivo, as well as their application in target (in)validation. We also highlight the importance of wisely selecting chemical probes and encourage best practices in using such tool compounds.
期刊介绍：
ACS Pharmacology & Translational Science publishes high quality, innovative, and impactful research across the broad spectrum of biological sciences, covering basic and molecular sciences through to translational preclinical studies. Clinical studies that address novel mechanisms of action, and methodological papers that provide innovation, and advance translation, will also be considered. We give priority to studies that fully integrate basic pharmacological and/or biochemical findings into physiological processes that have translational potential in a broad range of biomedical disciplines. Therefore, studies that employ a complementary blend of in vitro and in vivo systems are of particular interest to the journal. Nonetheless, all innovative and impactful research that has an articulated translational relevance will be considered.
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